Antibiotic AX-127B-1 is a relatively new aminoglycoside antibiotic. (Commonly assigned, co-pending U.S. Ser. No. 008,378, filed Feb. 1, 1979).
Chemical modification of the aminoglycoside antibiotics, as with other classes of antibiotics, has been found to improve the activity, either intrinsic or against resistant strains of organisms, or to reduce the toxicity of the parent antibiotics. And, because of the development of aminoglycoside-resistant strains and inactivation of the parent antibiotics by R-mediated factors which can develop, the search continues for new entities which are either superior to known aminoglycosides or which provide an alternative therapy when resistant organisms develop.
In a related family of aminoglycoside antibiotics, the fortimicins, 3-O-demethylation has been found to improve the intrinsic activity of the antibiotics. See, for example, U.S. Pat. No. 4,124,756.
3-O-demethyl-antibiotic AX-127B-1 and its 4-N-alkyl and acyl derivatives are disclosed and claimed in commonly assigned, copending U.S. Ser. No. 126,732, filed Mar. 3, 1980, now U.S. Pat. No. 4,283,529. The present invention provides derivatives of antibiotic AX-127B-1 which are useful as intermediates in the preparation of the 3-O-demethyl derivatives of AX-127B-1, and, in some instances, are also useful as antibiotics and anti-bacterial agents.